RU2014147728A - DERIVATIVE TRANS-2-DECENIC ACID AND CONTAINING ITS MEDICINE - Google Patents

DERIVATIVE TRANS-2-DECENIC ACID AND CONTAINING ITS MEDICINE Download PDF

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RU2014147728A
RU2014147728A RU2014147728A RU2014147728A RU2014147728A RU 2014147728 A RU2014147728 A RU 2014147728A RU 2014147728 A RU2014147728 A RU 2014147728A RU 2014147728 A RU2014147728 A RU 2014147728A RU 2014147728 A RU2014147728 A RU 2014147728A
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substituted
alkyl
pharmaceutical agent
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pharmaceutically acceptable
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RU2014147728A
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RU2602810C2 (en
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Мунеказу ИИНУМА
Соеи ФУРУКАВА
Мицуру НАИКИ
Томонори МАЦУМОТО
Кунихико ХИГАСИУРА
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Ниппон Дзоки Фармасьютикал Ко., Лтд.
Нагоя Индастриал Сайенс Рисерч Инститьют
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Abstract

1. Производное транс-2-деценовой кислоты, представленное следующей общей формулой (I') или его фармацевтически приемлемая соль:,где X' представляет собой:(a) 1-пирролидил, замещенный карбоксилом или алкоксикарбонилом,(b) 3-тиазолидил,(c) пиперидино, замещенный алкилом, оксо, гидрокси, алкокси, карбоксилом, алкоксикарбонилом, алкиламино, алкиламиноалкилом, фенилом, карбоксиалкилом, алкоксикарбонилалкилом, циано или галогенофенилом,(d) тиоморфолино,(e) 1-пиперазил, который может быть замещен алкилом, карбоксиалкилом, алкоксикарбонилалкилом, алкиламиноалкилом, циклоалкилом, пиперидиноалкилом, фенилалкилом, пиридилом, пиримидилом, карбоксифенилалкилом или алкоксикарбонилфенилалкилом,(f) 1-пиперазил, замещенный фенилом, который может быть замещен алкиламино, галогеном, алкокси, алкилом, гидрокси, карбоксиалкокси или алкоксикарбонилалкокси,(g) 1,4-диазепанил, который может быть замещен алкилом или алкиламиноалкилом, или(h) карбоксиморфолино.2. Производное транс-2-деценовой кислоты или его фармацевтически приемлемая соль по п. 1, где X' представляет собой 1-пирролидил, замещенный карбоксилом или алкоксикарбонилом.3. Производное транс-2-деценовой кислоты или его фармацевтически приемлемая соль по п. 1, где X' представляет собой 3-тиазолидил, тиоморфолино или карбоксиморфолино.4. Производное транс-2-деценовой кислоты или его фармацевтически приемлемая соль по п. 1, где X' представляет собой пиперидино, замещенный алкилом, оксо, гидрокси, алкокси, карбоксилом, алкоксикарбонилом, алкиламино, алкиламиноалкилфенилом, карбоксиалкилом, алкоксикарбонилалкилом, циано или галогенофенилом.5. Производное транс-2-деценовой кислоты или его фармацевтически приемлемая соль по п. 1, где X' пре1. A trans-2-decenoic acid derivative represented by the following general formula (I ′) or a pharmaceutically acceptable salt thereof: wherein X ′ is: (a) 1-pyrrolidyl substituted with carboxyl or alkoxycarbonyl, (b) 3-thiazolidyl, (c) piperidino substituted with alkyl, oxo, hydroxy, alkoxy, carboxyl, alkoxycarbonyl, alkylamino, alkylaminoalkyl, phenyl, carboxyalkyl, alkoxycarbonylalkyl, cyano or halogenophenyl, (d) thiomorpholino, (e) 1-piperazyl, which may be substituted carboxyalkyl, alkoxycarbonylalkyl, alkyl n-alkyl, cycloalkyl, piperidinoalkyl, phenylalkyl, pyridyl, pyrimidyl, carboxyphenylalkyl or alkoxycarbonylphenylalkyl, (f) 1-piperazyl substituted by phenyl, which may be substituted by alkylamino, halogen, alkoxy, alkoxyalkylalkyl, alkyl -diazepanyl, which may be substituted by alkyl or alkylaminoalkyl, or (h) carboxymorpholino. 2. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof according to claim 1, wherein X 'is 1-pyrrolidyl substituted with carboxyl or alkoxycarbonyl. 3. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof according to claim 1, wherein X 'is 3-thiazolidyl, thiomorpholino or carboxymorpholino. 4. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof according to claim 1, wherein X ′ is piperidino substituted with alkyl, oxo, hydroxy, alkoxy, carboxyl, alkoxycarbonyl, alkylamino, alkylaminoalkylphenyl, carboxyalkyl, alkoxycarbonylalkyl, cyano or halo phenyl. . Derivative of trans-2-decenoic acid or its pharmaceutically acceptable salt according to claim 1, where X 'pre

Claims (16)

1. Производное транс-2-деценовой кислоты, представленное следующей общей формулой (I') или его фармацевтически приемлемая соль:1. A trans-2-decenoic acid derivative represented by the following general formula (I ′) or a pharmaceutically acceptable salt thereof:
Figure 00000001
,
Figure 00000001
,
где X' представляет собой:where X 'represents: (a) 1-пирролидил, замещенный карбоксилом или алкоксикарбонилом,(a) 1-pyrrolidyl substituted with carboxyl or alkoxycarbonyl, (b) 3-тиазолидил,(b) 3-thiazolidyl, (c) пиперидино, замещенный алкилом, оксо, гидрокси, алкокси, карбоксилом, алкоксикарбонилом, алкиламино, алкиламиноалкилом, фенилом, карбоксиалкилом, алкоксикарбонилалкилом, циано или галогенофенилом,(c) piperidino substituted with alkyl, oxo, hydroxy, alkoxy, carboxyl, alkoxycarbonyl, alkylamino, alkylaminoalkyl, phenyl, carboxyalkyl, alkoxycarbonylalkyl, cyano or halogenophenyl, (d) тиоморфолино,(d) thiomorpholino, (e) 1-пиперазил, который может быть замещен алкилом, карбоксиалкилом, алкоксикарбонилалкилом, алкиламиноалкилом, циклоалкилом, пиперидиноалкилом, фенилалкилом, пиридилом, пиримидилом, карбоксифенилалкилом или алкоксикарбонилфенилалкилом,(e) 1-piperazyl, which may be substituted by alkyl, carboxyalkyl, alkoxycarbonylalkyl, alkylaminoalkyl, cycloalkyl, piperidinoalkyl, phenylalkyl, pyridyl, pyrimidyl, carboxyphenylalkyl or alkoxycarbonylphenylalkyl, (f) 1-пиперазил, замещенный фенилом, который может быть замещен алкиламино, галогеном, алкокси, алкилом, гидрокси, карбоксиалкокси или алкоксикарбонилалкокси,(f) 1-piperazyl substituted with phenyl which may be substituted with alkylamino, halogen, alkoxy, alkyl, hydroxy, carboxyalkoxy or alkoxycarbonylalkoxy, (g) 1,4-диазепанил, который может быть замещен алкилом или алкиламиноалкилом, или(g) 1,4-diazepanyl, which may be substituted by alkyl or alkylaminoalkyl, or (h) карбоксиморфолино.(h) carboxymorpholino.
2. Производное транс-2-деценовой кислоты или его фармацевтически приемлемая соль по п. 1, где X' представляет собой 1-пирролидил, замещенный карбоксилом или алкоксикарбонилом.2. A derivative of trans-2-decenoic acid or a pharmaceutically acceptable salt thereof according to claim 1, wherein X 'is 1-pyrrolidyl substituted with carboxyl or alkoxycarbonyl. 3. Производное транс-2-деценовой кислоты или его фармацевтически приемлемая соль по п. 1, где X' представляет собой 3-тиазолидил, тиоморфолино или карбоксиморфолино.3. A derivative of trans-2-decenoic acid or a pharmaceutically acceptable salt thereof according to claim 1, wherein X 'is 3-thiazolidyl, thiomorpholino or carboxymorpholino. 4. Производное транс-2-деценовой кислоты или его фармацевтически приемлемая соль по п. 1, где X' представляет собой пиперидино, замещенный алкилом, оксо, гидрокси, алкокси, карбоксилом, алкоксикарбонилом, алкиламино, алкиламиноалкилфенилом, карбоксиалкилом, алкоксикарбонилалкилом, циано или галогенофенилом.4. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof according to claim 1, wherein X ′ is piperidino substituted with alkyl, oxo, hydroxy, alkoxy, carboxyl, alkoxycarbonyl, alkylamino, alkylaminoalkylphenyl, carboxyalkyl, alkoxycarbonylalkyl, cyano or halo . 5. Производное транс-2-деценовой кислоты или его фармацевтически приемлемая соль по п. 1, где X' представляет собой 1-пиперазил, который может быть замещен алкилом, карбоксиалкилом, алкоксикарбонилалкилом, алкиламиноалкилом, циклоалкилом, пиперидиноалкилом, фенилалкилом, пиридилом, пиримидилом, карбоксифенилалкилом или алкоксикарбонилфенилалкилом.5. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof according to claim 1, wherein X ′ is 1-piperazyl, which may be substituted by alkyl, carboxyalkyl, alkoxycarbonylalkyl, alkylaminoalkyl, cycloalkyl, piperidinoalkyl, phenylalkyl, pyridyl, pyrimidyl carboxyphenylalkyl or alkoxycarbonylphenylalkyl. 6. Производное транс-2-деценовой кислоты или его фармацевтически приемлемая соль по п. 1, где X' представляет собой 1-пиперазил, замещенный фенилом, который может быть замещен алкиламино, галогеном, алкокси, алкилом, гидрокси, карбоксиалкокси или алкоксикарбонилалкокси.6. A trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof according to claim 1, wherein X 'is 1-piperazyl substituted with phenyl, which may be substituted with alkylamino, halogen, alkoxy, alkyl, hydroxy, carboxyalkoxy or alkoxycarbonylalkoxy. 7. Производное транс-2-деценовой кислоты или его фармацевтически приемлемая соль по п. 1, где X' представляет собой 1,4-диазепанил, который может быть замещен алкилом или алкиламиноалкилом.7. A derivative of trans-2-decenoic acid or a pharmaceutically acceptable salt thereof according to claim 1, wherein X 'is 1,4-diazepanyl, which may be substituted by alkyl or alkylaminoalkyl. 8. Фармацевтическое средство содержащее, в качестве активного ингредиента, по меньшей мере один член, выбранный из производного транс-2-деценовой кислоты, представленного следующей общей формулой (I), и его фармацевтически приемлемой соли:8. A pharmaceutical agent containing, as an active ingredient, at least one member selected from a trans-2-decene acid derivative represented by the following general formula (I) and a pharmaceutically acceptable salt thereof:
Figure 00000002
,
Figure 00000002
,
где X представляет собой:where X represents: (a) 1-пирролидил, замещенный карбоксилом или алкоксикарбонилом,(a) 1-pyrrolidyl substituted with carboxyl or alkoxycarbonyl, (b) 3-тиазолидил,(b) 3-thiazolidyl, (c) пиперидино, замещенный алкилом, оксо, гидрокси, алкокси, карбоксилом, алкоксикарбонилом, алкиламино, алкиламиноалкилом, фенилом, карбоксиалкилом, алкоксикарбонилалкилом, циано или галогенофенилом,(c) piperidino substituted with alkyl, oxo, hydroxy, alkoxy, carboxyl, alkoxycarbonyl, alkylamino, alkylaminoalkyl, phenyl, carboxyalkyl, alkoxycarbonylalkyl, cyano or halogenophenyl, (d) тиоморфолино,(d) thiomorpholino, (e) 1-пиперазил, который может быть замещен алкилом, карбоксиалкилом, алкоксикарбонилалкилом, алкиламиноалкилом, циклоалкилом, пиперидиноалкилом, фенилалкилом, пиридилом, пиримидилом, карбоксифенилалкил или алкоксикарбонилфенилалкилом,(e) 1-piperazyl, which may be substituted by alkyl, carboxyalkyl, alkoxycarbonylalkyl, alkylaminoalkyl, cycloalkyl, piperidinoalkyl, phenylalkyl, pyridyl, pyrimidyl, carboxyphenylalkyl or alkoxycarbonylphenylalkyl, (f) 1-пиперазил, замещенный фенилом, который может быть замещен алкиламино, галогеном, алкокси, алкилом, гидрокси, карбоксиалкокси или алкоксикарбонилалкокси,(f) 1-piperazyl substituted with phenyl which may be substituted with alkylamino, halogen, alkoxy, alkyl, hydroxy, carboxyalkoxy or alkoxycarbonylalkoxy, (g) 1,4-диазепанил, который может быть замещен алкилом или алкиламиноалкилом, или(g) 1,4-diazepanyl, which may be substituted by alkyl or alkylaminoalkyl, or (h) карбоксиморфолино.(h) carboxymorpholino.
9. Фармацевтическое средство по п. 8, где фармацевтическое средство представляет собой профилактическое средство или терапевтическое средство от расстройств периферической нервной системы, вызванных введением лекарственного средства, включающего по меньшей мере одно противораковое средство.9. The pharmaceutical agent of claim 8, wherein the pharmaceutical agent is a prophylactic or therapeutic agent for disorders of the peripheral nervous system caused by the administration of a drug comprising at least one anticancer agent. 10. Фармацевтическое средство по п. 8, где фармацевтическое средство представляет собой профилактическое средство или терапевтическое средство от нейродегенеративных заболеваний.10. The pharmaceutical agent according to claim 8, wherein the pharmaceutical agent is a prophylactic or therapeutic agent for neurodegenerative diseases. 11. Фармацевтическое средство по п. 8, где фармацевтическое средство представляет собой профилактическое средство или терапевтическое средство от психических заболеваний.11. The pharmaceutical agent of claim 8, wherein the pharmaceutical agent is a prophylactic or therapeutic agent for mental illness. 12. Фармацевтическое средство по п. 11, где психические заболевания представляют собой депрессию, тревожные расстройства (неврозы) или расстройства аутистического спектра.12. The pharmaceutical agent of claim 11, wherein the mental illness is depression, anxiety disorder (neurosis), or autism spectrum disorder. 13. Фармацевтическое средство по п. 8, где фармацевтическое средство представляет собой анальгетик против болевых синдромов.13. The pharmaceutical agent of claim 8, wherein the pharmaceutical agent is an analgesic against pain syndromes. 14. Фармацевтическое средство по любому одному из пп. 8-13, где фармацевтическое средство представляет собой препарат для инъекций.14. The pharmaceutical agent according to any one of paragraphs. 8-13, where the pharmaceutical agent is an injectable preparation. 15. Фармацевтическое средство по любому одному из пп. 8-13, где фармацевтическое средство представляет собой пероральный препарат.15. The pharmaceutical agent according to any one of paragraphs. 8-13, where the pharmaceutical agent is an oral preparation. 16. Фармацевтическое средство по любому одному из пп. 8-13, где фармацевтическое средство представляет собой средство для наружного применения. 16. The pharmaceutical agent according to any one of paragraphs. 8-13, where the pharmaceutical agent is an external agent.
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